Referencia número: HY-17040

Darunavir

(Synonyms: TMC114; UIC-94017)

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC₅₀ = 0.003 μM; IC₉₀ = 0.009 μM) with minimal cytotoxicity.

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Pureza: 99.91%
No. CAS: 206361-99-1
Fòrmula: C₂₇H₃₇N₃O₇S
Peso molecular:547.66

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Darunavir Chemical Structure

No. CAS: 206361-99-1

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (17)
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Actividad biológica

Descripciòn

IC₅₀ & Target

HIV-1

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Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	EC₅₀	10 nM Compound: DRV	Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	6 nM Compound: DRV	Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	8 nM Compound: DRV	Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	9 nM Compound: DRV	Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
HEK293	EC₅₀	0.15 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.18 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.23 nM Compound: 2, DRV	Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.25 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.3 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.6 nM Compound: 2, DRV	Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK-293T	CC₅₀	>100 μM Compound: DRV	Cytotoxicity against human 293T cells measured after 24 hrs by CCK8 assay Cytotoxicity against human 293T cells measured after 24 hrs by CCK8 assay	[PMID: 31734023]
HEK-293T	CC₅₀	>100 μM Compound: DRV	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33906049]
HEK-293T	CC₅₀	>100 μM Compound: DRV	Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay	[PMID: 35483138]
HEK-293T	CC₅₀	>200 μM Compound: DRV	Cytotoxicity against human HEK-293T cells after 24 hrs by CCK-8 assay Cytotoxicity against human HEK-293T cells after 24 hrs by CCK-8 assay	[PMID: 35278855]
HEK-293T	CC₅₀	61 μM Compound: DRV	Cytotoxicity against HEK293T cells incubated for 48 hrs by absorbance based assay Cytotoxicity against HEK293T cells incubated for 48 hrs by absorbance based assay	[PMID: 37244161]
HEK-293T	EC₅₀	13660 nM Compound: darunavir	Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay	[PMID: 22148316]
HepG2	CC₅₀	95.5 μM Compound: 2, TMC-114	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
MDCK-II	IC₅₀	>100 μM Compound: DRV	Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells	[PMID: 17664327]
MT2	CC₅₀	>100 μM Compound: 2, TMC-114	Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
MT2	CC₅₀	>100 μM Compound: DRV	Cytotoxicity against human MT2 cells after 7 days by MTT assay Cytotoxicity against human MT2 cells after 7 days by MTT assay	[PMID: 20439612]
MT2	CC₅₀	83.1 μM Compound: darunavir, DRV	Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.0039 μM Compound: darunavir, DRV	Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.0068 μM Compound: darunavir, DRV	Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.008 μM Compound: darunavir, DRV	Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.008 μM Compound: DRV	Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.01 μM Compound: DRV	Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	2.3 nM Compound: 2, TMC-114	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay	10.1039/C1MD00147G
MT2	IC₅₀	0.003 μM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT2 cells assessed as inhibition of p24 Gag protein production Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT2 cells assessed as inhibition of p24 Gag protein production	[PMID: 21800876]
MT2	IC₅₀	0.0034 μM Compound: DRV, darunavir	Antiviral activity against HIV1 LAI in MT2 cells Antiviral activity against HIV1 LAI in MT2 cells	[PMID: 17635930]
MT2	IC₅₀	1.6 nM Compound: 1, DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 19746963]
MT2	IC₅₀	3 nM Compound: 2, DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 23947685]
MT2	IC₅₀	3 nM Compound: Darunavir	Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay	[PMID: 26096678]
MT2	IC₅₀	3 nM Compound: 1, TMC-114	Antiviral activity against HIV1 LAI isolate in human MT2 cells Antiviral activity against HIV1 LAI isolate in human MT2 cells	[PMID: 16913714]
MT2	IC₅₀	3 nM Compound: DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells Antiviral activity against HIV1 LAI infected in human MT2 cells	[PMID: 26306007]
MT4	CC₅₀	>10 μM Compound: Darunavir	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 23177258]
MT4	CC₅₀	9.8 μM Compound: 1, DPV	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	>100 nM Compound: DPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay	[PMID: 18212102]
MT4	EC₅₀	0.0026 μM Compound: DRV	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	0.003 μM Compound: darunavir, DRV	Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.0033 μM Compound: darunavir, DRV	Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.0034 μM Compound: darunavir, DRV	Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.0035 μM Compound: DRV	Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay	[PMID: 26107245]
MT4	EC₅₀	0.0058 μM Compound: darunavir, DRV	Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.006 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.009 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.009 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.015 μM Compound: darunavir, DRV	Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.016 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.018 μM Compound: darunavir, DRV	Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.019 μM Compound: DRV	Antiviral activity against multidrug resistant HIV1 MDR/C containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production Antiviral activity against multidrug resistant HIV1 MDR/C containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production	[PMID: 26107245]
MT4	EC₅₀	0.021 μM Compound: darunavir, DRV	Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.023 μM Compound: DRV	Antiviral activity against multidrug resistant HIV1 MDR/G containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production Antiviral activity against multidrug resistant HIV1 MDR/G containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production	[PMID: 26107245]
MT4	EC₅₀	0.025 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.028 μM Compound: DRV	Antiviral activity against multidrug resistant HIV1 MDR/B containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production Antiviral activity against multidrug resistant HIV1 MDR/B containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production	[PMID: 26107245]
MT4	EC₅₀	0.029 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.031 μM Compound: DRV	Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	0.036 μM Compound: darunavir, DRV	Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.097 μM Compound: DRV	Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	0.2 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.21 μM Compound: darunavir, DRV	Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.29 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.33 μM Compound: darunavir, DRV	Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	11 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	11 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	11.3 nM Compound: 1, DPV	Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	12 nM Compound: DPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay	[PMID: 18212102]
MT4	EC₅₀	12 nM Compound: DRV	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 17576848]
MT4	EC₅₀	12 nM Compound: DRV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	12 nM Compound: Darunavir	Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	15 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	17 nM Compound: Darunavir	Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma	[PMID: 23177258]
MT4	EC₅₀	17.2 nM Compound: 1, DPV	Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum	[PMID: 24900331]
MT4	EC₅₀	19 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	2.3 nM Compound: 1, DPV	Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	2.4 nM Compound: Darunavir	Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	22 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	3.5 μM Compound: DRV	Antiviral activity against darunavir-resistant HIV1 P51 infected in human MT4 cells by XTT assay Antiviral activity against darunavir-resistant HIV1 P51 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	338 nM Compound: DPV	Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas	[PMID: 18212102]
MT4	EC₅₀	338 nM Compound: DRV	Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	4 nM Compound: DRV	Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay	[PMID: 19961222]
MT4	EC₅₀	40 nM Compound: DPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay	[PMID: 18212102]
MT4	EC₅₀	5.6 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	51 nM Compound: 1, DPV	Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	51 nM Compound: Darunavir	Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	515 nM Compound: DRV	Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	587 nM Compound: DPV	Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio	[PMID: 18212102]
MT4	EC₅₀	587 nM Compound: DRV	Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	6.6 nM Compound: 1, DPV	Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	6.6 nM Compound: Darunavir	Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	857 nM Compound: DPV	Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in	[PMID: 18212102]
MT4	IC₅₀	10 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	11 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	130 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	16 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	22 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	25 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	3 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	3.2 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	3.9 nM Compound: TMC-114	Antiviral activity against HIV1 HXB2 in MT4 cells Antiviral activity against HIV1 HXB2 in MT4 cells	[PMID: 16458505]
MT4	IC₅₀	30 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	32 nM Compound: TMC-114	Antiviral activity against HIV D545701 in MT4 cells Antiviral activity against HIV D545701 in MT4 cells	[PMID: 16458505]
MT4	IC₅₀	6.8 nM Compound: TMC-114	Antiviral activity against HIV1 EP13 in MT4 cells Antiviral activity against HIV1 EP13 in MT4 cells	[PMID: 16458505]
PBMC	EC₅₀	>0.025 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-JSL infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-JSL infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.0037 μM Compound: 2, DRV	Antiviral activity against wild type HIV1 ERS104pre infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production Antiviral activity against wild type HIV1 ERS104pre infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production	[PMID: 23947685]
PBMC	EC₅₀	0.0038 μM Compound: 9; DRV	Antiviral activity against wild type HIV1 ERS104pre infected in human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against wild type HIV1 ERS104pre infected in human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.004 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.0043 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-TM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-TM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.005 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-C infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-C infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.007 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-G infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-G infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.008 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.01 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-MM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-MM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.01 μM Compound: 2, DRV	Antiviral activity against multidrug-resistant HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production Antiviral activity against multidrug-resistant HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production	[PMID: 23947685]
PBMC	EC₅₀	0.011 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.019 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.019 μM Compound: 2, DRV	Antiviral activity against multidrug-resistant HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production. Antiviral activity against multidrug-resistant HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production.	[PMID: 23947685]
PBMC	EC₅₀	0.021 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-B infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-B infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.023 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.024 μM Compound: 2, DRV	Antiviral activity against multidrug-resistant HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production Antiviral activity against multidrug-resistant HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production	[PMID: 23947685]
PBMC	EC₅₀	0.027 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	255.2 nM Compound: 9; DRV	Antiviral activity against darunavir-resistant HIV1 20P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against darunavir-resistant HIV1 20P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	43.4 nM Compound: 9; DRV	Antiviral activity against darunavir-resistant HIV1 10P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against darunavir-resistant HIV1 10P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	IC₅₀	10.2 nM Compound: 1, TMC-114	Antiviral activity against multi drug-resistant HIV1 B variant in human PHA-PBMC cells Antiviral activity against multi drug-resistant HIV1 B variant in human PHA-PBMC cells	[PMID: 16913714]
PBMC	IC₅₀	3 nM Compound: 1, TMC-114	Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells	[PMID: 16913714]
PBMC	IC₅₀	3.5 nM Compound: 1, TMC-114	Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells	[PMID: 16913714]
PBMC	IC₅₀	3.5 nM Compound: 1, TMC-114	Antiviral activity against multi drug-resistant HIV1 TM variant in human PHA-PBMC cells Antiviral activity against multi drug-resistant HIV1 TM variant in human PHA-PBMC cells	[PMID: 16913714]
PBMC	IC₅₀	3.7 nM Compound: 1, TMC-114	Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells	[PMID: 16913714]
SUP-T1	EC₅₀	0.0025 μM Compound: DRV	Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by	[PMID: 35483138]
TZM	CC₅₀	>100 μM Compound: DRV	Cytotoxicity against human TZM-bl cells incubated for 48 hrs by absorbance based assay Cytotoxicity against human TZM-bl cells incubated for 48 hrs by absorbance based assay	[PMID: 37244161]
Vero C1008	EC₅₀	>40 μM Compound: Darunavir	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days	10.1101/2020.04.03.023846

In Vitro

Darunavir (TMC114, 1a) has a stability comparable to other protease inhibitors^[1].
Darunavir (TMC114, UIC-94017) blocks the infectivity and replication of each of HIV-1_NL4-3 variants exposed to and selected for resistance to Ro 31-8959, MK-639, AG1341, or ABT 538 at concentrations up to 5 μM (IC₅₀s, 0.003 to 0.029 μM), although it was less active against HIV-1_NL4-3 variants selected for resistance to VX-478 (IC₅₀, 0.22 μM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 206361-99-1
Appearance Solid
Peso molecular 547.66
Fòrmula C₂₇H₃₇N₃O₇S
Color White to off-white
SMILES

O=C(O[C@@H]1[C@@]2([H])[C@@](OCC2)([H])OC1)N[C@@H](CC3=CC=CC=C3)[C@H](O)CN(S(=O)(C4=CC=C(N)C=C4)=O)CC(C)C
Synonyms

TMC114; UIC-94017
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

All

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Journal Impact Factor

Signal Transduct Target Ther

Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]

2021 May 29;6(1):212. PMID: 34052830
Nat Microbiol

Superinfection promotes replication and diversification of defective HIV-1 proviruses in people with non-suppressible viraemia. [Abstract]

2025 Nov;10(11):2736-2748. PMID: 41044362
Nat Commun

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]

2020 Sep 4;11(1):4417. PMID: 32887884
Cell Rep Med

Decoupling HIV-1 antiretroviral drug inhibition from plasma antibody activity to evaluate broadly neutralizing antibody therapeutics and vaccines. [Abstract]

2024 Aug 26:101702. PMID: 39216479
Aging Cell

Antiretroviral protease inhibitors induce features of cellular senescence that are reversible upon drug removal. [Abstract]

2023 Jan;22(1):e13750. PMID: 36539941
Pharmaceuticals (Basel)

Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices. [Abstract]

2022 Feb 18;15(2):242. PMID: 35215354
J Photochem Photobiol A Chem

2025 Nov 15;473:116930.
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Antimicrob Agents Chemother

Discovery of M Protease Inhibitors Encoded by SARS-CoV-2. [Abstract]

2020 Aug 20;64(9):e00872-20. PMID: 32669265
ACS Omega

Highly Potent Phosphinic HIV‑1 Protease Inhibitors: Synthesis, In Vitro Evaluation, and Docking Studies. [Abstract]

2025 Dec 10;10(50):62083-62098. PMID: 41476560
Antiviral Res

HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway. [Abstract]

2022 Dec:208:105463. PMID: 36372295
Mol Divers

A potent and selective PROTAC degrader of CDK9 as effective inhibitor of HIV-1 RNA synthesis. [Abstract]

2025 Nov 12. PMID: 41225073
J Neuroimmune Pharmacol

Antiretroviral Drugs Promote Amyloidogenesis by De-Acidifying Endolysosomes. [Abstract]

2021 Mar;16(1):159-168. PMID: 31338753
J Chem

2025 Oct 15.
bioRxiv

Superinfection with intact HIV-1 results in conditional replication of defective proviruses and nonsuppressible viremia in people living with HIV-1. [Abstract]

2025 Apr 4:2025.04.04.647291. PMID: 40236094
Research Square Print

2022 May.
bioRxiv

2020 Apr.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (182.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8260 mL

9.1298 mL

18.2595 mL

5 mM

0.3652 mL

1.8260 mL

3.6519 mL

10 mM

0.1826 mL

0.9130 mL

1.8260 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Dominique L N G Surleraux, et al. Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. J Med Chem. 2005 Mar 24;48(6):1813-22. [Content Brief]

[2]. Yasuhiro Koh, et al. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob Agents Chemother. 2003 Oct;47(10):3123-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8260 mL	9.1298 mL	18.2595 mL	45.6488 mL
	5 mM	0.3652 mL	1.8260 mL	3.6519 mL	9.1298 mL
	10 mM	0.1826 mL	0.9130 mL	1.8260 mL	4.5649 mL
	15 mM	0.1217 mL	0.6087 mL	1.2173 mL	3.0433 mL
	20 mM	0.0913 mL	0.4565 mL	0.9130 mL	2.2824 mL
	25 mM	0.0730 mL	0.3652 mL	0.7304 mL	1.8260 mL
	30 mM	0.0609 mL	0.3043 mL	0.6087 mL	1.5216 mL
	40 mM	0.0456 mL	0.2282 mL	0.4565 mL	1.1412 mL
	50 mM	0.0365 mL	0.1826 mL	0.3652 mL	0.9130 mL
	60 mM	0.0304 mL	0.1522 mL	0.3043 mL	0.7608 mL
	80 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5706 mL
	100 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4565 mL

Keywords

Darunavir

17 Cited Publications

100 mg Obtener un presupuesto

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Darunavir

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Peptidomimetic Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Darunavir

Ver todos los productos específicos de isoformas HIV

Actividad biológica

Chemical Information

Publications (17)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Darunavir

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Peptidomimetic Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Darunavir

Ver todos los productos específicos de isoformas HIV

Actividad biológica

Chemical Information

Publications (17)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Darunavir Related Classifications

Referencia número: HY-17040